2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl-sulfonamide derivatives
Abstract
The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.
Claims
exact text as granted — not AI-modified1 . A 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being
(A) a compound of the formula I
wherein
R 1 is hydrogen, halogen, C 1-4 alkyl, C 1-4 halogenalkyl, C 3-4 cycloalkyl or C 3-4 halogencycloalkyl;
R 2 is a group selected from the group consisting of
R 8 is hydrogen; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the nitrogen atom of the group A1 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the nitrogen atom of the group A1 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
R 9 and R 10 independently are hydrogen or fluoro;
m is 1 or 2;
n is 0, 1, 2 or 3;
R 11 is halogen; cyano; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A2 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A2 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
p is 1 or 2;
q is 0, 1, 2 or 3;
R 12 is hydrogen, halogen, C 1-3 alkyl, C 1-3 halogenalkyl or cyclopropyl; and R 13 is hydrogen;
or R 12 and R 13 are independently halogen or methyl;
or R 12 and R 13 together with the carbon atom to which they are bound form a cyclopropyl;
R 14 is halogen; cyano; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A3 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A3 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
R 15 and R 16 independently are hydrogen; halogen; cyano; C 1-6 alkyl; C 1-6 haloalkyl;
C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A4 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A4 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
or R 15 and R 16 together with the carbon atom to which they are bound form a C 3-6 cycloalkyl;
R 17 is C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the oxygen atom of the group A4 or via a C 1-2 alkylene, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; or phenyl, wherein the phenyl may be attached directly to the oxygen atom of the group A4 or via a C 1-2 alkylene, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl;
R 18 and R 19 independently are hydrogen; halogen; cyano; C 1-6 alkyl; C 1-6 haloalkyl;
C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A5 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A5 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
or R 18 and R 19 together with the carbon atom to which they are bound form a C 3-6 cycloalkyl;
R 20 is hydrogen, halogen, C 1-3 alkyl, C 1-3 halogenalkyl or cyclopropyl; and R 21 is hydrogen;
or R 20 and R 21 are independently halogen or methyl;
or R 20 and R 21 together with the carbon atom to which they are bound form a cyclopropyl;
or R 18 and R 20 together with the adjacent carbon atoms to which they are bound form a C 3-6 cycloalkyl; and R 19 and R 21 are hydrogen;
R 22 is C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the oxygen atom of the group A5 or via a C 1-2 alkylene, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; or phenyl, wherein the phenyl may be attached directly to the oxygen atom of the group A5 or via a C 1-2 alkylene, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl;
R 3 is C 1-4 halo genalkyl, C 1-4 alkyl, C 3-4 cycloalkyl, C 3-4 halogencycloalkyl, halogen or nitro;
R 4 is hydrogen or fluoro;
R 5 is C 1-4 alkyl; C 1-4 halogenalkyl; C 2-4 alkenyl; C 2-4 halogenalkenyl; C 2-4 alkinyl;
C 2-4 halogenalkinyl; or a three- to seven-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain from 1 to 4 hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur, wherein the ring system may contain not more than 2 oxygen atoms and not more than 2 sulfur atoms, wherein the ring system may be substituted once or more than once by C 1-4 alkyl, C 1-4 halogenalkyl, C 1-4 alkoxy, C 1-4 halogenalkoxy, halogen or cyano, wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen, and wherein the ring system may be directly attached to the sulfur atom or via a C 1-4 alkylene group;
R 6 is C 1-10 alkylcarbonyl which may be substituted once or more than once by R 23 , C 3-6 cycloalkylcarbonyl which may be substituted once or more than once by R 24 , phenylcarbonyl which may be substituted once or more than once by R 25 , C 3-6 cycloalkyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 26 , phenyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 27 ; C 1-10 alkoxycarbonyl which may be substituted once or more than once by R 28 , or C 3-6 cycloalkoxycarbonyl which may be substituted once or more than once by R 29 ; phenyloxycarbonyl which may be substituted once or more than once by R 30 , C 3-6 cycloalkyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 31 , phenyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 32 ;
R 7 is hydrogen, C 1-10 alkylcarbonyl which may be substituted once or more than once by R 33 , C 3-6 cycloalkylcarbonyl which may be substituted once or more than once by R 34 , phenylcarbonyl which may be substituted once or more than once by R 35 , C 3-6 cycloalkyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 36 , phenyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 37 ; C 1-10 alkoxycarbonyl which may be substituted once or more than once by R 38 , or C 3-6 cycloalkoxycarbonyl which may be substituted once or more than once by R 39 ; phenyloxycarbonyl which may be substituted once or more than once by R 40 , C 3-6 cycloalkyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 41 , phenyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 42 ;
each R 23 , R 24 , R 25 , R 26 , R 27 , R 28 , R 29 , R 30 , R 31 , R 32 , R 33 , R 34 , R 35 , R 36 , R 37 , R 38 , R 39 , R 40 , R 41 and R 42 independently is C 1-6 alkoxy, C 1-4 alkoxy-C 1-6 alkoxy, phenoxy, phenyl-C 1-2 alkoxy, C 1-6 alkylthio, C 1-6 alkoxycarbonyl, C 1-6 alkylcarbonyloxy or morpholin-4-yl;
in free form or in salt form; or
(B) a compound selected from the group consisting of
4-[(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-amino]-4-oxo-butyric acid ethyl ester;
N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-pentanoyl-methanesulfonamide;
N-Acetyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-propionyl-methanesulfonamide;
N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-isobutyryl-methanesulfonamide;
N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-(3-methyl-butyryl)-methanesulfonamide;
N-Cyclopentanecarbonyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
N-Hexanoyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
N-Butyryl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid ethyl ester;
N-Butyryl-N-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide;
Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid propyl ester;
Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isobutyl ester;
N-(2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-propionyl-methanesulfonamide;
N-Butyryl-N-(2,4-dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
Acetic acid 2-[(2,4-dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-amino]-2-oxo-ethyl ester;
(2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-carbamic acid methyl ester;
(2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-carbamic acid ethyl ester;
N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-(3-methyl-butyryl)-methanesulfonamide;
N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-hexanoyl-methanesulfonamide;
N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-pentanoyl-methanesulfonamide;
N-Butyryl-N-(2,4-dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide;
N-Hexanoyl-N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide;
Methanesulfonyl-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid 2-methoxy-ethyl ester;
N-Butyryl-N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide;
N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-isobutyryl-methanesulfonamide; and
N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide;
in free form or in salt form.
2 . A 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative according to claim 1 wherein said derivative is a compound of the formula I
wherein
R 1 is hydrogen, halogen, C 1-4 alkyl, C 1-4 halogenalkyl, C 3-4 cycloalkyl or C 3-4 halogencycloalkyl;
R 2 is a group selected from the group consisting of
R 8 is hydrogen; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the nitrogen atom of the group A1 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the nitrogen atom of the group A1 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
R 9 and R 10 independently are hydrogen or fluoro;
m is 1 or 2;
n is 0, 1, 2 or 3;
R 11 is halogen; cyano; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A2 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A2 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
p is 1 or 2;
q is 0, 1, 2 or 3;
R 12 is hydrogen, halogen, C 1-3 alkyl, C 1-3 halogenalkyl or cyclopropyl; and R 13 is hydrogen;
or R 12 and R 13 are independently halogen or methyl;
or R 12 and R 13 together with the carbon atom to which they are bound form a cyclopropyl;
R 14 is halogen; cyano; hydroxy; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl;
C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A3 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A3 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
R 15 and R 16 independently are hydrogen; halogen; cyano; C 1-6 alkyl; C 1-6 haloalkyl;
C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A4 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A4 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
or R 15 and R 16 together with the carbon atom to which they are bound form a C 3-6 cycloalkyl;
R 17 is C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the oxygen atom of the group A4 or via a C 1-2 alkylene, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; or phenyl, wherein the phenyl may be attached directly to the oxygen atom of the group A4 or via a C 1-2 alkylene, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl;
R 18 and R 19 independently are hydrogen; halogen; cyano; C 1-6 alkyl; C 1-6 haloalkyl;
C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the carbon atom of the group A5 or via a C 1-2 alkylene or an oxygen, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; phenyl, wherein the phenyl may be attached directly to the carbon atom of the group A5 or via a C 1-2 alkylene or an oxygen, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl; C 1-6 alkoxy; or C 1-6 haloalkoxy;
or R 18 and R 19 together with the carbon atom to which they are bound form a C 3-6 cycloalkyl;
R 20 is hydrogen, halogen, C 1-3 alkyl, C 1-3 halogenalkyl or cyclopropyl; and R 21 is hydrogen;
or R 20 and R 21 are independently halogen or methyl;
or R 20 and R 21 together with the carbon atom to which they are bound form a cyclopropyl;
or R 18 and R 20 together with the adjacent carbon atoms to which they are bound form a C 3-6 cycloalkyl; and R 19 and R 21 are hydrogen;
R 22 is C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; C 1-4 alkoxy-C 1-4 alkyl; C 3-6 cycloalkyl, wherein one carbon atom may be replaced by an oxygen atom, wherein the C 3-6 cycloalkyl may be attached directly to the oxygen atom of the group A5 or via a C 1-2 alkylene, and wherein the C 3-6 cycloalkyl may be substituted by halogen, hydroxy or C 1-4 alkyl; or phenyl, wherein the phenyl may be attached directly to the oxygen atom of the group A5 or via a C 1-2 alkylene, and wherein the phenyl may be substituted by halogen, hydroxy or C 1-4 alkyl;
R 3 is C 1-4 halogenalkyl, C 1-4 alkyl, C 3-4 cycloalkyl, C 3-4 halogencycloalkyl, halogen or nitro;
R 4 is hydrogen or fluoro;
R 5 is C 1-4 alkyl; C 1-4 halogenalkyl; C 2-4 alkenyl; C 2-4 halogenalkenyl; C 2-4 alkinyl; C 2-4 halogenalkinyl; or a three- to seven-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain from 1 to 4 hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur, wherein the ring system may contain not more than 2 oxygen atoms and not more than 2 sulfur atoms, wherein the ring system may be substituted once or more than once by C 1-4 alkyl, C 1-4 halogenalkyl, C 1-4 alkoxy, C 1-4 halogenalkoxy, halogen or cyano, wherein a substituent on a nitrogen in a heterocyclic ring system may not be halogen, and wherein the ring system may be directly attached to the sulfur atom or via a C 1-4 alkylene group;
R 6 is C 1-10 alkylcarbonyl which may be substituted once or more than once by R 23 , C 3-6 cycloalkylcarbonyl which may be substituted once or more than once by R 24 , phenylcarbonyl which may be substituted once or more than once by R 25 , C 3-6 cycloalkyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 26 , phenyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 27 ; C 1-10 alkoxycarbonyl which may be substituted once or more than once by R 28 , or C 3-6 cycloalkoxycarbonyl which may be substituted once or more than once by R 29 ; phenyloxycarbonyl which may be substituted once or more than once by R 30 ;
C 3-6 cycloalkyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 31 , phenyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 32 ;
R 7 is hydrogen, C 1-10 alkylcarbonyl which may be substituted once or more than once by R 33 , C 3-6 cycloalkylcarbonyl which may be substituted once or more than once by R 34 , phenylcarbonyl which may be substituted once or more than once by R 35 , C 3-6 cycloalkyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 36 , phenyl-C 1-2 alkylcarbonyl which may be substituted once or more than once by R 37 ; C 1-10 alkoxycarbonyl which may be substituted once or more than once by R 38 , or C 3-6 cycloalkoxycarbonyl which may be substituted once or more than once by R 39 ; phenyloxycarbonyl which may be substituted once or more than once by R 40 ;
C 3-6 cycloalkyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 41 , phenyl-C 1-2 alkoxycarbonyl which may be substituted once or more than once by R 42 ; each R 23 , R 24 , R 25 , R 26 , R 27 , R 28 , R 29 , R 30 , R 31 , R 32 , R 33 , R 34 , R 35 , R 36 , R 37 , R 38 , R 39 , R 40 , R 41 and R 42 independently is C 1-6 alkoxy, C 1-4 alkoxy-C 1-6 alkoxy, phenoxy, phenyl-C 1-2 alkoxy, C 1-6 alkylthio, C 1-6 alkoxycarbonyl, C 1-6 alkylcarbonyloxy or morpholin-4-yl.
3 . A compound of formula I according to claim 2 , wherein R 1 is hydrogen.
4 . A compound of formula I according to claim 2 , wherein R 2 is a group A2; R 8 is C 1-6 alkyl; and R 9 and R 10 independently are hydrogen or fluoro.
5 . A compound of formula I according to claim 2 , wherein R 3 is C 1-4 halogenalkyl or C 1-4 alkyl.
6 . A compound of formula I according to claim 2 , wherein R 5 is C 1-4 alkyl.
7 . A compound of formula I according to claim 2 , wherein R 6 is C 1-10 alkylcarbonyl which may be substituted once or more than once by R 23 ; R 7 is hydrogen or C 1-10 alkylcarbonyl which may be substituted once or more than once by R 33 ; and each R 23 and R 33 independently is C 1-6 alkoxy or C 1-6 alkylthio.
8 . A 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative according to claim 1 , wherein said 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative is selected from the group consisting of
N-[6-(2-Methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; N-Isobutyryl-N-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Butyryl-N-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Hexanoyl-N-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; Methanesulfonyl-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid methyl ester; Methanesulfonyl-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isobutyl ester; Methanesulfonyl-[6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid 2-methoxy-ethyl ester; N-Acetyl-N-[7-ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Butyryl-N-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-hexanoyl-methanesulfonamide; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isobutyl ester; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid 2-methoxy-ethyl ester; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid propyl ester; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid methyl ester; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid ethyl ester; Methanesulfonyl-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid butyl ester; N-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; N-[7-Ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; Methanesulfonyl-[7-ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isopropyl ester; Methanesulfonyl-[7-ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid pentyl ester; N-Acetyl-N-[1-acetyl-7-ethyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Acetyl-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid 2-methoxy-ethyl ester; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid isobutyl ester; 3-(Isobutoxycarbonyl-methanesulfonyl-amino)-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid isobutyl ester; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid methyl ester; 4-{[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-4-oxo-butyric acid ethyl ester; 3-{[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-3-oxo-propionic acid ethyl ester; 5-{[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-5-oxo-pentanoic acid ethyl ester; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; Acetic acid 2-{[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-1,1-dimethyl-2-oxo-ethyl ester; Acetic acid 2-[3-[(2-acetoxy-2-methyl-propionyl)-methanesulfonyl-amino]-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl]-1,1-dimethyl-2-oxo-ethyl ester; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; N-Butyryl-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Hexanoyl-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Decanoyl-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Isobutyryl-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; Acetic acid 2-{[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-2-oxo-ethyl ester; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-(3-methylsulfanyl-propionyl)-methanesulfonamide; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid ethyl ester; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid propyl ester; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid butyl ester; [7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid hexyl ester; N-(2,2-Dimethyl-propionyl)-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Acetyl-N-[1-acetyl-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1-propionyl-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; N-Butyryl-N-[1-butyryl-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; [1-Acetyl-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid benzyl ester; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-{2-[2-(2-methoxy-ethoxy)-ethoxy]-acetyl}-methane sulfonamide; N-(2-Benzyloxy-acetyl)-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-(4-Benzyloxy-butyryl)-N-[7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-(2-morpholin-4-yl-acetyl)-methanesulfonamide; 7-Isopropyl-3-(methoxycarbonyl-methanesulfonyl-amino)-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid methyl ester; 3-(Ethoxycarbonyl-methanesulfonyl-amino)-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid ethyl ester; 7-Isopropyl-3-(methanesulfonyl-propoxycarbonyl-amino)-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid propyl ester; 3-(Butoxycarbonyl-methanesulfonyl-amino)-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid butyl ester; 3-(Acetyl-methanesulfonyl-amino)-7-isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-3,4-dihydro-2H-quinazoline-1-carboxylic acid methyl ester; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-(4-morpholin-4-yl-butyryl)-methanesulfonamide; N-[7-Isopropyl-6-(2-methyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-(3-morpholin-4-yl-propionyl)-methanesulfonamide; 4-[(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-amino]-4-oxo-butyric acid ethyl ester; N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-pentanoyl-methanesulfonamide; N-Acetyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-propionyl-methanesulfonamide; N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-isobutyryl-methanesulfonamide; N-(6-Imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-(3-methyl-butyryl)-methanesulfonamide; N-Cyclopentanecarbonyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-Hexanoyl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-Butyryl-N-(6-imidazol-1-yl-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-Acetyl-N-[6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; N-Butyryl-N-[6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Hexanoyl-N-[6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Isobutyryl-N-[6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; [6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid ethyl ester; [6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid propyl ester; [6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid butyl ester; [6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid isobutyl ester; [6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid 2-methoxy-ethyl ester; 5-{[6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-5-oxo-pentanoic acid ethyl ester; 3-{[6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-3-oxo-propionic acid ethyl ester; N-[6-(2-Isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-(3-methylsulfanyl-propionyl)-methanesulfonamide; N-Acetyl-N-[7-difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Butyryl-N-[7-difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[7-Difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; [7-Difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid propyl ester; N-[7-Difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; [7-Difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid ethyl ester; [7-Difluoromethyl-6-(2-isopropyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid 2-methoxy-ethyl ester; Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid ethyl ester; N-Butyryl-N-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid propyl ester; Methanesulfonyl-[6-(2-methyl-imidazol-1-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isobutyl ester; N-(2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-propionyl-methanesulfonamide; N-Butyryl-N-(2,4-dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; Acetic acid 2-[(2,4-dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-amino]-2-oxo-ethyl ester; (2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-carbamic acid methyl ester; (2,4-Dioxo-6-pyrrol-1-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-carbamic acid ethyl ester; N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-(3-methyl-butyryl)-methanesulfonamide; N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-hexanoyl-methanesulfonamide; N-(2,4-Dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-pentanoyl-methanesulfonamide; N-Butyryl-N-(2,4-dioxo-6-[1,2,4]triazol-4-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-Acetyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-propionyl-methanesulfonamide; N-Butyryl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonamide; Methanesulfonyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-carbamic acid methyl ester; Methanesulfonyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-carbamic acid ethyl ester; Methanesulfonyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-carbamic acid butyl ester; Methanesulfonyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-carbamic acid 2-methoxy-ethyl ester; Methanesulfonyl-N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-carbamic acid isobutyl ester; N-(2,4-dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-hexanoyl-methanesulfonamide; 4-[(2,4-Dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-methanesulfonyl-amino]-4-oxo-butyric acid ethyl ester; N-(2,4-Dioxo-6-tetrahydro-furan-2-yl-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl)-N-pentanoyl-methanesulfonamide; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid 2-methoxy-ethyl ester; N-[6-(1-Methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid ethyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid propyl ester; N-Hexanoyl-N-[6-(1-Methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Isobutyryl-N-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Butyryl-N-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-Acetyl-N-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid methyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isobutyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid butyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid pentyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid hexyl ester; Methanesulfonyl-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid isopropyl ester; N-[6-(1-methoxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; N-Hexanoyl-N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; Methanesulfonyl-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-carbamic acid 2-methoxy-ethyl ester; N-Butyryl-N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-isobutyryl-methanesulfonamide; N-[6-(1-hydroxy-propyl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-pentanoyl-methanesulfonamide; Methanesulfonyl-[7-Ethyl-6-(2-ethyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]carbamic acid isobutyl ester; N-[7-Ethyl-6-(2-ethyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-hexanoyl-methanesulfonamide; N-[7-Ethyl-6-(2-ethyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; Acetic acid 2-{[7-difluoromethyl-6-(2-ethyl-2H-pyrazol-3-yl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-amino}-2-oxo-ethyl ester; [6-(2-Ethyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid methyl ester; N-[6-(2-Ethyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-N-propionyl-methanesulfonamide; [6-(2-Ethyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonyl-carbamic acid butyl ester; and N-(2,2-Dimethyl-propionyl)-N-[6-(2-ethyl-2H-pyrazol-3-yl)-2,4-dioxo-7-trifluoromethyl-1,4-dihydro-2H-quinazolin-3-yl]-methanesulfonamide; and wherein said 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative is in free form or in salt form.
9 . A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and one or more pharmaceutically acceptable carriers.
10 . A combination comprising a therapeutically effective amount of the compound according to claim 1 and one or more therapeutically active agents.
11 . A method of inhibiting AMPA- and/or kainate-receptor activity in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 1 .
12 . A method of treating a disorder or a disease in a subject mediated by AMPA- and/or kainate-receptors in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 1 .
13 - 15 . (canceled)
16 . A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 2 and one or more pharmaceutically acceptable carriers.
17 . A combination comprising a therapeutically effective amount of the compound according to claim 2 and one or more therapeutically active agents.
18 . A method of inhibiting AMPA- and/or kainate-receptor activity in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 2 .
19 . A method of treating a disorder or a disease mediated by AMPA- and/or kainate-receptors in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 2 .
20 . A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 8 and one or more pharmaceutically acceptable carriers.
21 . A combination comprising a therapeutically effective amount of the compound according to claim 8 and one or more therapeutically active agents.
22 . A method of inhibiting AMPA- and/or kainate-receptor activity in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 8 .
23 . A method of treating a disorder or a disease mediated by AMPA- and/or kainate-receptors in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 8 .Join the waitlist — get patent alerts
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